C07K1/113

STAPLED AND STITCHED POLYPEPTIDES AND USES THEREOF
20220372075 · 2022-11-24 ·

The present invention provides stapled polypeptides of the Formulae (I) and (VI):

##STR00001##

and salts thereof; wherein the groups custom-character; R.sup.1a, R.sup.1b, R.sup.1c, R.sup.2a, R.sup.3a, R.sup.2b, R.sup.3b, R.sup.4a, R.sup.4b, R.sub.A, R.sub.Z, L.sub.1a, L.sub.1b, L.sub.2, L.sub.3, X.sup.AA, v, w, p, m, s, n, t, and q are as defined herein. The present invention further provides methods of preparing the inventive stapled polypeptides from unstapled polypeptide precursors. The present invention further provides pharmaceutical compositions comprising a stapled polypeptide of Formula (I) or (VI), and methods of using the stapled peptides. The present invention also provides modifications of the staples post ring closing metathesis.

STAPLED AND STITCHED POLYPEPTIDES AND USES THEREOF
20220372075 · 2022-11-24 ·

The present invention provides stapled polypeptides of the Formulae (I) and (VI):

##STR00001##

and salts thereof; wherein the groups custom-character; R.sup.1a, R.sup.1b, R.sup.1c, R.sup.2a, R.sup.3a, R.sup.2b, R.sup.3b, R.sup.4a, R.sup.4b, R.sub.A, R.sub.Z, L.sub.1a, L.sub.1b, L.sub.2, L.sub.3, X.sup.AA, v, w, p, m, s, n, t, and q are as defined herein. The present invention further provides methods of preparing the inventive stapled polypeptides from unstapled polypeptide precursors. The present invention further provides pharmaceutical compositions comprising a stapled polypeptide of Formula (I) or (VI), and methods of using the stapled peptides. The present invention also provides modifications of the staples post ring closing metathesis.

METHODS OF CONJUGATING AN AGENT TO A THIOL MOIETY IN A PROTEIN THAT CONTAINS AT LEAST ONE TRISULFIDE BOND

The invention provides improved methods of conjugating an agent to a thiol moiety in a protein that contains at least one disulfide bond and at least one trisulfide bond. Exemplary embodiments include the production of antibody drug conjugates substantially free of impurities created in the presence of reactive sulfide moieties in the production processes.

CELL PENETRATING STAPLED PEPTIDE, MANUFACTURING METHOD THEREFOR, AND USE THEREOF
20170342108 · 2017-11-30 ·

The present invention relates to a stapled peptide, a preparation method thereof and the use thereof, and more specifically to an amphipathic alpha-helical stapled peptide comprising hydrophobic amino acids and hydrophilic amino acids, a preparation method thereof, and the use thereof for intracellular delivery of an active substance.

Conjugated polymeric material and uses thereof

Disclosed are compositions comprising collagen covalently bound to particles, wherein covalent bonds are formed between reactive groups of the collagen and reactive groups of the particles, and wherein the particles have an average particle diameter ranging from 20 to 1000 nanometers. Also disclosed are various methods that utilize the compositions.

Method for preparing crystalline insulin

A method for crystallizing insulin or insulin analogs under alkaline conditions and purifying the insulin or insulin analog crystals by filtering through a filter and drying the insulin or insulin analog crystals captured on the filter to produce crystalline insulin or insulin analog crystal compositions is described. In particular aspects, the method may be used to crystalize insulin glargine.

METHODS FOR SYNTHESIZING alpha4ß7 PEPTIDE ANTAGONISTS

The present invention provides methods of making α4β7 peptide monmer and dimer antagonists. Methods of the present invention include solid phase and solution phase methods, as well as synthesis via condensation of smaller peptide fragments. Methods of the present invention further include methods directed to the synthesis of peptides comprising one or more penicillamine residues.

Anti-VEGF protein compositions and methods for producing the same

The present disclosure pertains to compositions comprising anti-VEGF proteins and methods for producing such compositions.

Anti-VEGF protein compositions and methods for producing the same

The present disclosure pertains to compositions comprising anti-VEGF proteins and methods for producing such compositions.

BIOLOGICALLY ACTIVE PEPTIDOMIMETIC MACROCYCLES

The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.